钙黄绿素脂质体的细胞转运及其机制研究

厉群,吴赛伟,梁文权,孙晓译*

中国药学杂志 ›› 2014, Vol. 49 ›› Issue (15) : 1321-1326.

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中国药学杂志 ›› 2014, Vol. 49 ›› Issue (15) : 1321-1326. DOI: 10.11669/cpj.2014.15.012
论著

钙黄绿素脂质体的细胞转运及其机制研究

  • 厉群1,吴赛伟1,梁文权2,孙晓译3*
作者信息 +

Cellular Delivery of Liposomal Calcein and Its Mechanism Study

  • LI Qun1, WU Sai-wei1, LIANG Wen-quan2, SUN Xiao-yi3*
Author information +
文章历史 +

摘要

目的 研究钙黄绿素脂质体的细胞转运及其入胞机制。方法 用薄膜分散法制备钙黄绿素脂质体,比较钙黄绿素水溶液和脂质体的体外释放过程,研究脂质体包裹对钙黄绿素在A549细胞内蓄积、分布和入胞途径的影响。结果 钙黄绿素脂质体具有良好的缓释作用,可释放长达1周。相对于钙黄绿素水溶液,脂质体包裹使被动跨膜的钙黄绿素通过大胞饮和网格蛋白(clathrin)介导的内吞途径入胞,大幅度提高钙黄绿素入胞量,主要分布于溶酶体内。结论 小分子水溶性药物可以通过脂质体包裹改变入胞途径,提高入胞能力,影响胞内分布。该结论为研究载有水溶性药物脂质体的细胞递送过程,进一步合理设计脂质体处方提供参考和依据。

Abstract

OBJECTIVE To investigate the cellular delivery of calcein-loaded liposomes and the endocytosis mechanism. METHODS Liposomes were prepared by film dispersion method. The in vitro release profiles of calcein solution and calcein loaded liposomes were compared via dialysis method, and the effects of liposome encapsulation on the cellular accumulation, intracellular distribution and uptake mechanism of calcein were investigated on A549 cells. RESULTS The in vitro release test showed sustained release of calcein from liposomes, which lasted for 1 week. Liposomes significantly increased the amount of total and intracellular calcein (P<0.01), and calcein distributed mainly in the lysosomes and outside of the nucleus. The mechanism study showed that liposomes transferred calcein into cells mainly by macropinocytosis and clathrin-dependent endocytic pathway. CONCLUSION Liposome encapsulation can increase the amount of intracellular calcein by changing the endocytic pathway of calcein. Liposome encapsulation is a potential and feasible way for enhancing cellular delivery.

关键词

缓释 / 细胞摄取 / 大胞饮 / clathrin介导内吞 / 钙黄绿素

Key words

sustained release / cellular uptake / macropinocytosis / clathrin-dependent endocytosis / calcein

引用本文

导出引用
厉群,吴赛伟,梁文权,孙晓译*. 钙黄绿素脂质体的细胞转运及其机制研究[J]. 中国药学杂志, 2014, 49(15): 1321-1326 https://doi.org/10.11669/cpj.2014.15.012
LI Qun, WU Sai-wei, LIANG Wen-quan, SUN Xiao-yi*. Cellular Delivery of Liposomal Calcein and Its Mechanism Study[J]. Chinese Pharmaceutical Journal, 2014, 49(15): 1321-1326 https://doi.org/10.11669/cpj.2014.15.012
中图分类号: R944    R969   

参考文献

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基金

国家自然科学基金资助项目(30873176);浙江省自然科学基金资助项目(LQ12H30004);浙江省医药卫生科技计划(2012KYA067)
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